SB-222200 |
Catalog No.GC10107
One-Click Copy Product Info
|
An NK3 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 174635-69-9
Sample solution is provided at 25 µL, 10mM.
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SB 222200 is a selective and potent antagonist of NK-3 receptor [1].
Neurokinin-3 (NK-3) receptor is a member of the G-protein-coupled superfamily and functions as a receptor for tachykinin. Activation of NK-3 receptors causes phosphoinositol 4, 5 biphosphate
(PIP2) breakdown into 1,4,5 inositol triphosphate (IP3) and diacylglycerol through phospholipase C activation [1].
In Chinese hamster ovary (CHO) cell expressing the hNK-3 receptor, SB 222200 inhibited neurokinin B (NKB) binding to the cell membranes with a Ki value of 4.4 nM. In HEK 293 cells expressing the hNK-3 receptor, SB 222200 antagonized NKB-induced Ca2+ mobilization with an IC50 value of 18.4 nM [1].
In mice model, SB-222200 inhibited behavioral responses (rapid head shakes and tail whips) induced by senktide (the NK-3 receptor-selective agonist) with an ED50 value of 5 mg/kg in a dose-dependent way and the inhibitory effect correlated significantly with brain concentrations of SB-222200 [1]. Treatment adult male CD-1 mice with SB 222200, mice had significantly enhanced hyperactivity when challenged with cocaine, which suggested that blockade of NK-3 receptors enhanced dopamine-mediated behavioral hyperactivity.
References:
[1]. Sarau HM, Griswold DE, Bush B, et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther, 2000, 295(1): 373-381.
[2]. Nwaneshiudu CA, Unterwald EM. Blockade of neurokinin-3 receptors modulates dopamine-mediated behavioral hyperactivity. Neuropharmacology, 2009, 57(3): 295-301.
| Cas No. | 174635-69-9 | SDF | |
| Chemical Name | 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide | ||
| Canonical SMILES | CCC(C1=CC=CC=C1)NC(=O)C2=C(C(=NC3=CC=CC=C32)C4=CC=CC=C4)C | ||
| Formula | C26H24N2O | M.Wt | 380.48 |
| Solubility | ≥ 19.024 mg/mL in DMSO, ≥ 43.6 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL |
| 5 mM | 525.7 μL | 2.6283 mL | 5.2565 mL |
| 10 mM | 262.8 μL | 1.3141 mL | 2.6283 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)